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Assay Detail

CHEMBL687156

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
The compound was tested in vitro for inhibitory activity against HMG-CoA reductase
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

3-hydroxy-3-methylglutaryl-coenzyme A reductase (CHEMBL402)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 9. The synthesis and biological evaluation of novel simvastatin analogs.
Hartman GD, Halczenko W, Duggan ME, Imagire JS, Smith RL, Pitzenberger SM, Fitzpatrick SL, Alberts AW, Bostedor R, Chao YS.
J Med Chem (1992) 35 : 3813 -3821
PubMed 1433193 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.84 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3349827 1 8.12
CHEMBL3349828 1 7.97
CHEMBL3349544 1 7.92
CHEMBL3349824 1 7.88
CHEMBL333443 1 7.75
CHEMBL3349825 1 7.71
CHEMBL54440 MEVASTATIN 2.0 1 7.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3349827 IC50 = 7.6 nM 8.12
CHEMBL3349828 IC50 = 10.8 nM 7.97
CHEMBL3349544 IC50 = 12.1 nM 7.92
CHEMBL3349824 IC50 = 13.3 nM 7.88
CHEMBL333443 IC50 = 18.0 nM 7.75
CHEMBL3349825 IC50 = 19.7 nM 7.71
CHEMBL54440 MEVASTATIN IC50 = 28.4 nM 7.55